Evidence map›Paper›PMID 30375481›Full record

ArticleScientific reports2018

Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6.

Marta De Donato, Benedetta Righino, Flavia Filippetti, Alessandra Battaglia, Marco Petrillo, Davide Pirolli, Giovanni Scambia, Maria Cristina De Rosa, Daniela Gallo

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
2.5field-weighted citation impact, top 11% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

20 citing papers in PubMed, 36 citations in OpenAlex.

  1. Edge-Grafted Polyarginine Functionalization of Graphene Nanocarriers Maintains Noncovalent Aromatic Drug Loading.Journal of peptide science : an official publication of the European Peptide Society · 2026
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  12. In Mitosis You Are Not: The NIMA Family of Kinases inInternational journal of molecular sciences · 2022
    Review
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  14. Article
  15. Network Analysis Reveals Synergistic Genetic Dependencies for Rational Combination Therapy in Philadelphia Chromosome-Like Acute Lymphoblastic Leukemia.Clinical cancer research : an official journal of the American Association for Cancer Research · 2021
    Article
  16. Review
  17. Article
  18. Checking NEKs: Overcoming a Bottleneck in Human Diseases.Molecules (Basel, Switzerland) · 2020
    Review
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 2 institutions in 1 country.

Marta De DonatoInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Benedetta RighinoInstitute of Biochemistry and Clinical Biochemistry - Università Cattolica del Sacro Cuore, Rome, Italy.
Flavia FilippettiInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Alessandra BattagliaInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Marco PetrilloInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Davide PirolliInstitute of Chemistry of Molecular Recognition (ICRM) - CNR, Rome, Italy.
Giovanni ScambiaInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Maria Cristina De RosaInstitute of Chemistry of Molecular Recognition (ICRM) - CNR, Rome, Italy. mariacristina.derosa@icrm.cnr.it.ORCID http://orcid.org/0000-0002-9611-2490
Daniela GalloInstitute of Obstetrics and Gynecology, Università Cattolica del Sacro Cuore, Rome, Italy.
Università Cattolica del Sacro Cuore · ITInstitute of Chemistry of Molecular Recognition · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The NIMA (never in mitosis, gene A)-related kinase-6 (NEK6), which is implicated in cell cycle control and plays significant roles in tumorigenesis, is an attractive target for the development of novel anti-cancer drugs. Here we describe the discovery of a potent ATP site-directed inhibitor of NEK6 identified by virtual screening, adopting both structure- and ligand-based techniques. Using a homology-built model of NEK6 as well as the pharmacophoric features of known NEK6 inhibitors we identified novel binding scaffolds. Twenty-five compounds from the top ranking hits were subjected to in vitro kinase assays. The best compound, i.e. compound 8 ((5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile), was able to inhibit NEK6 with low micromolar IC

Indexed as

Drug DiscoveryAmino Acid SequenceAntineoplastic AgentsBinding SitesCell Line, TumorEnzyme ActivationHumansInhibitory Concentration 50LigandsMolecular ConformationMolecular Docking SimulationMolecular Dynamics SimulationMolecular StructureNIMA-Related KinasesProtein BindingProtein Interaction Domains and MotifsAntineoplastic AgentsLigandsNEK6 protein, humanNIMA-Related KinasesProtein Kinase Inhibitors

Identifiers

PMID30375481
PMCPMC6207720
OpenAlexW2898372196

What OpenQuestion holds

Textmetadata
LicenceCC BY
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.